947753-99-3Relevant academic research and scientific papers
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1)
Wilson, Kevin J.,Witter, David J.,Grimm, Jonathan B.,Siliphaivanh, Phieng,Otte, Karin M.,Kral, Astrid M.,Fleming, Judith C.,Harsch, Andreas,Hamill, Julie E.,Cruz, Jonathan C.,Chenard, Melissa,Szewczak, Alexander A.,Middleton, Richard E.,Hughes, Bethany L.,Dahlberg, William K.,Secrist, J. Paul,Miller, Thomas A.
, p. 1859 - 1863 (2008)
An HTS screening campaign identified a series of low molecular weight phenols that showed excellent selectivity (>100-fold) for HDAC1/HDAC2 over other Class I and Class II HDACs. Evolution and optimization of this HTS hit series provided HDAC1-selective (SHI-1) compounds with excellent anti-proliferative activity and improved physical properties. Dose-dependent efficacy in a mouse HCT116 xenograft model was demonstrated with a phenylglycine SHI-1 analog.
SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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Page/Page column 81, (2009/04/25)
The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation,
